Outputs (43)

The life cycle of the Mu-Opioid Receptor (2020)
Journal Article
Cuitavi, J., Hipólito, L., & Canals, M. (2021). The life cycle of the Mu-Opioid Receptor. Trends in Biochemical Sciences, 46(4), 315-328. https://doi.org/10.1016/j.tibs.2020.10.002

Opioid receptors are undisputed targets for the treatment of pain. Unfortunately, targeting these receptors therapeutically poses significant challenges including addiction, dependence, tolerance and the appearance of side-effects such as respiratory... Read More about The life cycle of the Mu-Opioid Receptor.

Critical assessment of G protein-biased agonism at the µ opioid receptor (2020)
Journal Article
Gillis, A., Kliewer, A., Kelly, E., Henderson, G., Christie, M. J., Schulz, S., & Canals, M. (2020). Critical assessment of G protein-biased agonism at the µ opioid receptor. Trends in Pharmacological Sciences, 41(12), 947-959. https://doi.org/10.1016/j.tips.2020.09.009

G protein-biased agonists of the µ-opioid receptor have been proposed to be an improved class of opioid analgesics. Recent studies have been unable to reproduce the original experiments in the β-arrestin2 knockout mouse that led to this proposal, and... Read More about Critical assessment of G protein-biased agonism at the µ opioid receptor.

Endosomal signaling of delta opioid receptors is an endogenous mechanism and therapeutic target for relief from inflammatory pain (2020)
Journal Article
Jimenez-Vargas, N. N., Gong, J., Wisdom, M. J., Jensen, D. D., Latorre, R., Hegron, A., Teng, S., DiCello, J. J., Rajasekhar, P., Veldhuis, N. A., Carbone, S. E., Yu, Y., Lopez-Lopez, C., Jaramillo-Polanco, J., Canals, M., Reed, D. E., Lomax, A. E., Schmidt, B. L., Leong, K. W., Vanner, S. J., …Poole, D. P. (2020). Endosomal signaling of delta opioid receptors is an endogenous mechanism and therapeutic target for relief from inflammatory pain. Proceedings of the National Academy of Sciences, 117(26), 15281-15292. https://doi.org/10.1073/pnas.2000500117

Whether G protein-coupled receptors signal from endosomes to control important pathophysiological processes and are therapeutic targets is uncertain. We report that opioids from the inflamed colon activate -opioid receptors (DOPr) in endosomes of noc... Read More about Endosomal signaling of delta opioid receptors is an endogenous mechanism and therapeutic target for relief from inflammatory pain.

Phosphoproteomic characterization of the signaling network resulting from activation of chemokine receptor CCR2 (2020)
Journal Article
Huang, C., Foster, S. R., Shah, A. D., Kleifeld, O., Canals, M., Schittenhelm, R. B., & Stone, M. J. (2020). Phosphoproteomic characterization of the signaling network resulting from activation of chemokine receptor CCR2. Journal of Biological Chemistry, 295, 6518-6531. https://doi.org/10.1074/jbc.ra119.012026

Leukocyte recruitment is a universal feature of tissue inflammation and regulated by the interactions of chemokines with their G protein-coupled receptors (GPCRs). Activation of CC chemokine receptor 2 (CCR2) by its cognate chemokine ligands, includi... Read More about Phosphoproteomic characterization of the signaling network resulting from activation of chemokine receptor CCR2.

Ligand-dependent spatiotemporal signaling profiles of the mu-opioid receptor are controlled by distinct protein-interaction networks (2019)
Journal Article
Civciristov, S., Huang, C., Liu, B., Marquez, E. A., Gondin, A. B., Schittenhelm, R. B., Ellisdon, A. M., Canals, M., & Halls, M. L. (2019). Ligand-dependent spatiotemporal signaling profiles of the mu-opioid receptor are controlled by distinct protein-interaction networks. Journal of Biological Chemistry, 294(44), 16198-16213. https://doi.org/10.1074/jbc.ra119.008685

Ligand-dependent differences in the regulation and internalization of the mu-opioid receptor (MOR) have been linked to the severity of adverse effects that limit opiate use in pain management. MOR activation by morphine or [D-Ala2,N-MePhe4,Gly-ol]-en... Read More about Ligand-dependent spatiotemporal signaling profiles of the mu-opioid receptor are controlled by distinct protein-interaction networks.

Influence of Chemokine N-Terminal Modification on Biased Agonism at the Chemokine Receptor CCR1 (2019)
Journal Article
Sanchez, J., Lane, R., Canals, M., & Stone, M. J. (2019). Influence of Chemokine N-Terminal Modification on Biased Agonism at the Chemokine Receptor CCR1. International Journal of Molecular Sciences, 20(10), 1-15. https://doi.org/10.3390/ijms20102417

Leukocyte migration, a hallmark of the inflammatory response, is stimulated by the interactions between chemokines, which are expressed in injured or infected tissues, and chemokine receptors, which are G protein-coupled receptors (GPCRs) expressed i... Read More about Influence of Chemokine N-Terminal Modification on Biased Agonism at the Chemokine Receptor CCR1.

GRK mediates μ-opioid receptor plasma membrane reorganization (2019)
Journal Article
Gondin, A. B., Halls, M. L., Canals, M., & Briddon, S. J. (2019). GRK mediates μ-opioid receptor plasma membrane reorganization. Frontiers in Molecular Neuroscience, 12, https://doi.org/10.3389/fnmol.2019.00104

Differential regulation of the μ-opioid receptor (MOP) has been linked to the development of opioid tolerance and dependence which both limit the clinical use of opioid analgesics. At a cellular level, MOP regulation occurs via receptor phosphorylati... Read More about GRK mediates μ-opioid receptor plasma membrane reorganization.

G protein-coupled receptors are dynamic regulators of digestion and targets for digestive diseases (2019)
Journal Article
Canals, M., Poole, D. P., Veldhuis, N. A., Schmidt, B. L., & Bunnett, N. W. (2019). G protein-coupled receptors are dynamic regulators of digestion and targets for digestive diseases. Gastroenterology, 156(6), 1600-1616. https://doi.org/10.1053/j.gastro.2019.01.266

G protein-coupled receptors (GPCRs) are the largest family of transmembrane signaling proteins. Within the gastrointestinal tract, GPCRs expressed by epithelial cells sense contents of the lumen, and GPCRs expressed by epithelial cells, myocytes, neu... Read More about G protein-coupled receptors are dynamic regulators of digestion and targets for digestive diseases.

Therapeutic targeting of HER2–CB2R heteromers in HER2-positive breast cancer (2019)
Journal Article
Blasco-Benito, S., Moreno, E., Seijo-Vila, M., Tundidor, I., Andradas, C., Caffarel, M. M., Caro-Villalobos, M., Urigüen, L., Diez-Alarcia, R., Moreno-Bueno, G., Hernández, L., Manso, L., Homar-Ruano, P., McCormick, P. J., Bibic, L., Bernadó-Morales, C., Arribas, J., Canals, M., Casadó, V., Canela, E. I., …Sánchez, C. (2019). Therapeutic targeting of HER2–CB2R heteromers in HER2-positive breast cancer. Proceedings of the National Academy of Sciences, 116(9), 3863-3872. https://doi.org/10.1073/pnas.1815034116

Although human epidermal growth factor receptor 2 (HER2)-targeted therapies have dramatically improved the clinical outcome of HER2-positive breast cancer patients, innate and acquired resistance remains an important clinical challenge. New therapeut... Read More about Therapeutic targeting of HER2–CB2R heteromers in HER2-positive breast cancer.

Hormones, neurotransmitters, growth factors, receptors, and signaling: Inflammation-associated changes in DOR expression and function in the mouse colon (2018)
Journal Article
Dicello, J., Saito, A., Rajasekhar, P., Eriksson, E., McQuade, R., Nowell, C., Sebastian, B., Fichna, J., Veldhuis, N., Canals, M., Bunnett, N., Carbone, S., & Poole, D. (2018). Hormones, neurotransmitters, growth factors, receptors, and signaling: Inflammation-associated changes in DOR expression and function in the mouse colon. American Journal of Physiology, 315(4), G544-G559. https://doi.org/10.1152/ajpgi.00025.2018

Endoge-nous opioids activate opioid receptors (ORs) in the enteric nervous system to control intestinal motility and secretion. The μ-OR mediates the deleterious side effects of opioid analgesics, including constipation, respiratory depression, and a... Read More about Hormones, neurotransmitters, growth factors, receptors, and signaling: Inflammation-associated changes in DOR expression and function in the mouse colon.